VprBP Inhibitor, B32B3

A cell permeable, potent, selective, and ATP-competitive inhibitor of Vpr (HIV-1) binding protein (VprBP) that preferentially targets cancer cells expressing VprBP and blocks phosphorylation of H2A at Thr120 (IC₅₀ = 500 nM in DU-145 human prostate cancer cells) and reduces cell proliferation. However, it has minimal effect on normal human prostate MLC cells lacking VprBP. Exhibits over 100-fold greater selectivity for VprBP over a panel of 33 other protein kinases. Shown to reduce xenograft tumor progression in nude mice injected with DU-145 cells (~5 mg/kg, i.p. twice a week for 3 weeks). Displays moderately desirable pharmacokinetic properties with t1/2= 7 h and Cmax of 1 µM.

A cell permeable, potent, selective, and ATP-competitive inhibitor of Vpr (HIV-1) binding protein (VprBP) that preferentially targets cancer cells expressing VprBP and blocks phosphorylation of H2A at Thr120 (IC₅₀ = 500 nM in DU-145 human prostate cancer cells) and reduces cell proliferation. However, it has minimal effect on normal human prostate MLC cells lacking VprBP. Exhibits over 100-fold greater selectivity for VprBP over a panel of 33 other protein kinases. Shown to reduce xenograft tumor progression in nude mice injected with DU-145 cells (~5 mg/kg, i.p. twice a week for 3 weeks). Displays moderately desirable pharmacokinetic properties with t1/2= 7 h and Cmax of 1 µM.

Please note that the molecular weight for this compound is batch-specific due to variable water content.

Cell permeable: yes

Primary Target
VprBP

Reversible: yes

Packaged under inert gas

Toxicity: Standard Handling (A)

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

Kim, K., et al. 2013. Mol. Cell.52, 459.

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany